A novel anti-platelet aggregation target of chinensinaphthol methyl ether and neojusticin B obtained from Rostellularia procumbens (L.) Nees

Abstract

This study explored the possible bioactive ingredients and target protein of Rostellularia procumbens (L.) Nees. The results of optical turbidimetry revealed that the ethyl acetate extraction obtained from R. procumbens (L.) Nees could inhibit platelet aggregation. Gene chip was used to investigate differentially expressed genes. According to the results of the gene chip, the targets of compounds isolated from the ethyl acetate extraction were predicted by network pharmacology. Computational studies revealed that chinensinaphthol methyl ether and neojusticin B may target the integrin α IIb β 3 protein. The results of Prometheus NT.48 and microscale thermophoresis suggested that the molecular interactions between the two compounds with purified integrin α IIb β 3 protein in the optimal test conditions were coherent with the docking results. To our best knowledge, this is the first report to state that chinensinaphthol methyl ether and neojusticin B target the integrin α IIb β 3 protein.

Extract from Rostellularia procumbens (L.) Nees Inhibits Thrombosis and Platelet Aggregation by Regulating Integrin β3 and MAPK Pathways

“…Integrin α IIb β 3 is the main receptor regulating platelet aggregation and thrombosis . Previous work done by our group found through the gene chip technology that the extract affected the expression of α IIb β 3 protein on platelets . Thus, it was suggested that the extract had the potential to develop into antiplatelet aggregation drugs.…”

“…procumbent (L.) Nees is a traditional herbal medicine with the efficacy of detoxicating, activating blood and pain relieving, diuretic swelling, and so on. Previous studies have demonstrated its efficacy in inhibiting platelet aggregation . However, it is not clear if R.…”

“…Previous studies have demonstrated its efficacy in inhibiting platelet aggregation. 14 However, it is not clear if R. procumbens (L.) Nees has any protective effects on thrombotic diseases. Therefore, in this study, we extracted the antithrombotic effective parts (RPE) and potential active parts (JAC) through the proven methods in the preliminary experiment in our lab.…”

Reveals of candidate active ingredients in Justicia and its anti-thrombotic action of mechanism based on network pharmacology approach and experimental validation

“…In addition, similar to Justicidin A, Justicidin B can selectively inhibit T helper 2 (Th2) cell responses in concanavalin A-activated spleen cells and polarized Th2 cells, thereby alleviating airway inflammation and bronchoconstriction 51 . Justicidin C, also called neojusticin B, has been reported to directly bind to integrin α IIb β 3 to inhibit platelet aggregation 52 . Therefore, based on the results of network analysis and combined with literature reports, justicidin D was used as a key focus in this work for experimental research.…”

Design, synthesis, and evaluation of cytotoxic activities of arylnaphthalene lignans and aza‐analogs

“…Natural arylnaphthalene lignans and analogs [1,2] continue to interest pharmaceutical industries owing to their biological activities. [3,4] Among them, arylnaphthalene lactones, which are present in a lot of plants often associated with traditional medicine use, are known to exhibit remarkable biological properties, especially antiproliferative, [5][6][7][8][9][10] antiviral, [11] antiplatelet, [12,13] and for this are considered as promising candidates for the elaboration of new drugs. [14] Natural products or analogs included in this family are classified into two types (A or B) related to the regio-orientation of the lactone ring (Figure 1).…”